In vitro functional characterization of A-278637
| Compound | Membrane Potential (FLIPR; −log EC50) Guinea Pig Bladder | Tissue Strip Relaxation1-a | ||
|---|---|---|---|---|
| Spontaneous Phasic Activity | Carbachol-Evoked Contractions | Electrical Field-Stimulated Contractions | ||
| −log IC50 | ||||
| A-278637 | 7.04 ± 0.11 (n = 5) | 7.64 ± 0.06 (n = 6) | 6.78 ± 0.08 (n = 6) | 6.51 ± 0.09 (n = 6) |
| 6.89 ± 0.33 (n = 7; human) | ||||
| WAY-133537 | 7.72 ± 0.06 (n = 6) | 6.99 ± 0.06 (n = 5) | 6.82 ± 0.01 (n = 6) | 6.17 ± 0.13 (n = 5) |
| ZD6169 | 6.56 ± 0.10 (n = 12) | 6.68 ± 0.11 (n = 3) | 6.87 ± 0.05 (n = 4) | 5.59 ± 0.09 (n = 6) |
↵1-a Data from pig detrusor strips except where indicated.